C([N:4]1[CH2:9][CH2:8][CH:7]([CH2:10][C:11]2[CH:16]=[CH:15][C:14]([S:17]([CH3:20])(=[O:19])=[O:18])=[CH:13][CH:12]=2)[CH2:6][CH2:5]1)(=O)C.[ClH:21]>>[ClH:21].[CH3:20][S:17]([C:14]1[CH:13]=[CH:12][C:11]([CH2:10][CH:7]2[CH2:6][CH2:5][NH:4][CH2:9][CH2:8]2)=[CH:16][CH:15]=1)(=[O:19])=[O:18]A mixture of 1-acetyl-4-[4-(methylsulfonyl)benzyl]-piperidine (8.76 g) and concentrated hydrochloric acid (100 mL) was stirred for 4 hours under reflux with heat. The reaction mixture was concentrated under reduced pressure. 2-Propanol (100 mL) was added thereto and the mixture was concentrated under reduced pressure. To the residue was added 2-propanol (50 mL), and the mixture was stirred under reflux with heat for 30 minutes and cooled down to room temperature. The precipitate was filtered off, washed with 2-propanol (50 mL) and dried under reduced pressure to give the title compound as a white solid (7.51 g).
Wird geladen…